A5071656162- Ion channel regulation and function
- Analytical Chemistry and Chromatography
- Cardiac electrophysiology and arrhythmias
- Neuroscience and Neuropharmacology Research
- Analytical Methods in Pharmaceuticals
- Asymmetric Synthesis and Catalysis
- Crystallization and Solubility Studies
- Computational Drug Discovery Methods
- Chemical synthesis and alkaloids
- Receptor Mechanisms and Signaling
- X-ray Diffraction in Crystallography
- Cholinesterase and Neurodegenerative Diseases
- Nicotinic Acetylcholine Receptors Study
- Cancer Treatment and Pharmacology
- Molecular spectroscopy and chirality
- Inorganic and Organometallic Chemistry
- Electrochemical Analysis and Applications
- Chemical Synthesis and Analysis
- Cancer therapeutics and mechanisms
- Pharmacogenetics and Drug Metabolism
- Innovative Microfluidic and Catalytic Techniques Innovation
- Synthesis and biological activity
- Genetic Neurodegenerative Diseases
- Synthetic Organic Chemistry Methods
- Free Radicals and Antioxidants
University of Bari Aldo Moro
2016-2025
Istituto di Farmacologia Traslazionale
2018
Institute of Crystallography
2012
Ospedale Buccheri la Ferla Fatebenefratelli
2012
University of Florence
2007
Drug-induced blockade of the human ether-à-go-go-related gene (hERG) channel is today considered main cause cardiotoxicity in postmarketing surveillance. Hence, several ligand-based approaches were developed last years and are currently employed early stages a drug discovery process for silico cardiac safety assessment candidates. Herein, we present first structure-based classifiers able to discern hERG binders from nonbinders. LASSO regularized support vector machines applied integrate...
Article10 March 2020Open Access Source DataTransparent process Targeting the pregnane X receptor using microbial metabolite mimicry Zdeněk Dvořák Corresponding Author [email protected] orcid.org/0000-0002-3938-3585 Department of Cell Biology and Genetics, Palacký University, Olomouc, Czech Republic Search for more papers by this author Felix Kopp Biochemistry, Albert Einstein College Medicine, Bronx, NY, USA Cait M Costello The Biological Environmental Engineering, Cornell Ithaca, Jazmin S...
Ultrasound-assisted extraction is widely recognized as an eco-friendly technique due to low solvent consumption and time well enhanced efficiency with respect conventional methods. Nevertheless, it would be convenient avoid the usually used organic solvents reduce environment pollution. In this regard, Deep Eutectic Solvents (DES) represent nowadays a green sustainable alternative for of bioactive compounds from natural sources. study, efficient stevioside rebaudioside A Stevia rebaudiana...
Thalidomide was first used for relief of morning sickness in pregnant women and then withdrawn from the market because its dramatic effects on normal fetal development. Over last decades, it has been successfully treatment several pathologies, including cancer. Many analogues with improved activity have synthesized tested. Herein we report some growth progression MCF-7 MDA-MB-231 breast cancer cells by a small series thalidomide-correlated compounds, which are very effective at inducing cell...
The desperate need to find drugs for COVID-19 has indicated repurposing strategies as our quickest way obtain efficacious medicines. One of the options under investigation is old antimalarial drug, chloroquine, and its analog, hydroxychloroquine. Developed synthetic succedanea cinchona alkaloids, these chiral antimalarials are currently in use racemate. Besides ethical concern related accelerated large-scale clinical trials with unproven efficacy, known potential detrimental cardiac effects...
Bamboo is a well-known medicinal plant in Southeast Asia that recently has attracted attention for its high polyphenol content and medical nutraceutical applications. In this work, polyphenols have been recovered the first time by microwave-assisted extraction (MAE) from an unusual Italian cultivar of Phyllostachys pubescens bamboo shoots. The effects three independent variables, such as time, temperature, solid/liquid ratio, on recovery yield were investigated successfully optimized through...
Leccinum scabrum (Bull.) Gray (Boletaceae) is an edible mycorrhizal species with potential application interest due to its food and medicinal properties. A field investigation carried out during summer in the Białowieża Primeval Forest, located along border between Belarus Poland allowed collect samples for chemical composition analysis antibacterial activity evaluation. Mushroom extracts were prepared microwave-assisted as well ultrasound-assisted extraction techniques (UAE MAE). The of a...
Among the alternative proteins aimed at replacing those of animal origin, fungal stand out as a promising resource capable meeting environmental, health, and ethical demands. Fungal biomasses, or mycoproteins, are indeed rich in other macro- micronutrients, while low fats. However, their production is an ongoing challenge. This study focused on submerged fermentation, highly controllable process that can couple high yields agro-industrial by-products exploitation growth media. Five medicinal...
Recently, nitrostilbenes characterized by two different or differently substituted aryl moieties, obtainable from the initial ring-opening of 3-nitrobenzo[b]thiophene with amines, have proved, means a stepwise double coupling phenolic-type bidentate C/O nucleophiles, to be valuable precursors oxygen-containing heteropolycycles and fully conjugated systems therefrom via an efficient 6π-electrocyclization final aromatization. Herein, methodology is extended, after suitable optimization,...
Xylazine, commonly called “tranq” or “sleep cut”, is a strong α2-adrenergic agonist used in veterinary practice as sedative, analgesic, and muscle-relaxing agent. It has never been approved by the Food Drug Administration for human use, but its use people on rise. In last decades, due to low cost ease of availability, it often illicitly abuse potential drug attempted sexual assault intended poisoning. addition, xylazine’s presence body also related domestic accidental events. Generally,...
The antioxidant, anti‐α‐glucosidase and anticholinesterase activity of the leaves rhizomatous extract Bergenia cordifolia were investigated. rhizomes that showed a higher degree 1,1‐diphenyl‐2‐picrylhydrazyl radical scavenging than reference compounds (rutin acarbose respectively) subjected to phytochemical analysis. study revealed previously unknown minor constituents from plant, (+)‐catechin 3‐ O ‐gallate, 3,5‐di‐ ‐gallate 1,2,4,6‐tetra‐ ‐galloyl‐β‐ d ‐glucopyranoside, principles. These as...
Citrus pomace is a huge agro-food industrial waste mostly composed of peels and traditionally used as compost or animal feed. Owing to its high content compounds beneficial humans (e.g., flavonoids, phenol-like acids, terpenoids), citrus increasingly produce valuable supplements, fragrance, antimicrobials. However, such processes require sustainable efficient extraction strategies by solvent-free techniques for environmentally-friendly good practices. In this work, we evaluated the...
The urgent need to increase the sustainability of crop production has pushed agricultural sector towards use biostimulants based on natural products. current work aimed determine whether preharvest application two commercial formulations, a Fabaceae enzymatic hydrolysate or blend nitrogen sources including fulvic acids, and lab-made aqueous extracts from Moringa oleifera leaves (MLEs), could improve yield, quality, storability lettuce grown in hydroponic system, as compared an untreated...
Medicinal plants belonging to the genus Berberis may be considered an interesting source of drugs counteract problem antimicrobial multiresistance. The important properties associated with this are mainly due presence berberine, alkaloid a benzyltetrahydroisoquinoline structure. Berberine is active against both Gram-negative and Gram-positive bacteria, influencing DNA duplication, RNA transcription, protein synthesis, integrity cell surface Countless studies have shown enhancement these...
Mexiletine is a sodium channel blocker, primarily used in the treatment of ventricular arrhythmias. Moreover, recent studies have demonstrated its therapeutic value to treat myotonic syndromes and relieve neuropathic pain. The present study aims at investigating direct blockade hERG potassium by mexiletine metabolite m-hydroxymexiletine (MHM). Our data show that inhibits time- voltage-dependent manner, with an IC50 3.7 ± 0.7 μmol/L. Analysis initial onset current inhibition during...